181375-13-3Relevant academic research and scientific papers
Synthesis and anti-MRSA activity of novel cephalosporin derivatives
D'Andrea, Stan V.,Bonner, Daniel,Bronson, Joanne J.,Clark, Junius,Denbleyker, Ken,Fung-Tomc, Joan,Hoeft, Shelley E.,Hudyma, Thomas W.,Matiskella, John D.,Miller, Raymond F.,Misco, Peter F.,Pucci, Michael,Sterzycki, Roman,Tsai, Yuan,Ueda, Yasutsuga,Wichtowski, John A.,Singh, Janak,Kissick, Thomas P.,North, Jeffery T.,Pullockaran, Annie,Humora, Michael,Boyhan, Brenda,Vu, Truc,Fritz, Alan,Heikes,Fox, Rita,Godfrey, Jollie D.,Perrone, Robert,Kaplan, Murray,Kronenthal, David,Mueller, Richard H.
, p. 5687 - 5698 (2007/10/03)
Cephalosporin derivatives containing a unique combination of lipophilic C-7 sidechains and polar C-3 thiopyridinium groups were synthesized and found to exhibit potent anti-MRSA activity in vitro and in vivo. The optimum C-7 sidechains utilized were 2,5-dichlorophenylthioacetamido and 2,6-dichloropyrid-4-ylthioacetamido. The C-3 thiopyridinium rings were substituted at nitrogen with amino acid and pyruvic acid groups that were designed to confer aqueous solubility as required for IV formulation. This paper describes the characteristics of these novel cephalosporins and highlights synthetic methods developed to allow their practical, large-scale syntheses. (C) 2000 Elsevier Science Ltd.
Synthesis and structure-activity relationship of C-3 quaternary ammonium cephalosporins exhibiting anti-MRSA activities
Kim, Oak K.,Hudyma, Thomas W.,Matiskella, John D.,Ueda, Yasutsugu,Bronson, Joanne J.,Mansuri, Muzammil M.
, p. 2753 - 2758 (2007/10/03)
A series of cephalosporins bearing C-3 quaternary ammonium groups were prepared and evaluated for their anti-MRSA activity. They exhibit good to excellent in vitro activity (MICs= 1-8 μg/mL) against MRSA.
Synthesis and structure-activity relationship of C-3 benzoyloxymethyl cephalosporins exhibiting anti-MRSA activities
Kim, Oak K.,Ueda, Yasutsugu,Mansuri, Muzammil M.,Russell, John W.,Bidwell, Valerie W.
, p. 1945 - 1950 (2007/10/03)
A series of cephalosporins bearing C-3 benzoyloxymethyl groups were prepared and evaluated for their anti-MRSA activity and plasma stability. They exhibit excellent in vitro activity (MIC = 0.06 ~ 2 μg/mL) against MRSA and excellent stability in human plasma.
